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Udenafil PDE inhibitor

Cat.No.S6433

Udenafil is a potent antagonist of human PDE5 with an IC50 of 8.25 nM and a comparable selectivity profile as sildenafil for the other PDEs.
Udenafil PDE inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 516.66

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S643301 DMSO]100 mg/mL]false]Ethanol]25 mg/mL]false]Water]Insoluble]false Purity: 99.99%
99.99

Chemical Information, Storage & Stability

Molecular Weight 516.66 Formula

C25H36N6O4S

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 268203-93-6 -- Storage of Stock Solutions

Synonyms N/A Smiles CCCC1=NN(C2=C1N=C(NC2=O)C3=C(C=CC(=C3)S(=O)(=O)NCCC4CCCN4C)OCCC)C

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (193.55 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 25 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Mechanism of Action

Targets/IC50/Ki
PDE5 [1]
(Cell-free assay)
8.25 nM
PDE3 [1]
(Cell-free assay)
52 nM
PDE6 [1]
(Cell-free assay)
53.3 nM
PDE2 [1]
(Cell-free assay)
101 nM
In vitro

The inhibitory effect of udenafil on PDE5 is about 150-fold greater than that on PDE1 (selectivity ratio of 149). PDE11 selectivity of this compound (selectivity ratio of 96) is relatively high, indicating a very low probability of inhibition of PDE11 at therapeutic doses of this chemical. The IC50 values for PDE2, PDE3, and PDE6 of this compound are 101±15.1 nM, 52.0±3.53 nM, and 53.3±2.47 nM respectively[1].
In vivo

Udenafil is rapidly absorbed, reaching peak plasma concentrations at 0.8-1.3 h, then declining monoexponentially with a terminal half-life (T1/2) between 7.3 and 12.1 hours, giving it the unique pharmacokinetics of both relatively rapid onset and long duration. This compound has also been shown in preclinical studies to have potent erectogenic properties in rats and rabbits with a broad safety margin[2]. Absolute oral bioavailability of this chemical is only 38% in rats. This low oral bioavailability appears to be mainly due to a considerable intestinal first-pass effect[1].
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01928563 Unknown status
Healthy Male Subjects
Dong-A Pharmaceutical Co. Ltd.|Dong-A ST Co. Ltd.
 September 2013 Phase 1
NCT01929213 Unknown status
Healthy Volunteers
Dong-A Pharmaceutical Co. Ltd.|Dong-A ST Co. Ltd.
 August 2013 Phase 1
NCT01108900 Completed
Erectile Dysfunction
Pfizer''s Upjohn has merged with Mylan to form Viatris Inc.|Pfizer
 July 2010 --

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